Cystine proportion regulates fate of polypeptide nanogel as nanocarrier for chemotherapeutics  

作　　者：Xiangru Feng Weiguo Xu Xiaoru Xu Gao Li Jianxun Ding Xuesi Chen 

机构地区：[1]Key Laboratory of Polymer Ecomaterials,Changchun Institute of Applied Chemistry,Chinese Academy of Sciences,Changchun,130022,China [2]School of Applied Chemistry and Engineering,University of Science and Technology of China,Hefei,230026,China [3]College of Acumox and Tuina,Changchun University of Chinese Medicine,Changchun,130022,China

出　　处：《Science China Chemistry》2021年第2期293-301,共9页中国科学（化学英文版）

基　　金：the National Natural Science Foundation of China(52022095,51973216,51873207,51803006,51833010,51673190,51603204);the Science and Technology Development Program of Jilin Province(20200404182YY);the Youth Talents Promotion Project of Jilin Province(181909);the Youth Innovation Promotion Association of Chinese Academy of Sciences(2019230)。

摘　　要：The physicochemical characteristics of nanoparticles are closely related to their drug delivery performances in vitro and in vivo.A well-designed nanocarrier can prolong the drug half-life in the blood circulation,upregulate the drug accumulation at the target site,and enhance the treatment efficacy.To elucidate the impact of physicochemical properties on the fate of nanogel as a nanocarrier of chemotherapeutics,three methoxy poly(ethylene glycol)-poly(L-phenylalanine-co-L-cystine)(mPEG-P(LP-coLC))nanogels with different L-cystine proportions were developed,namely mPEG-P(LP10-co-LC5)(NG10-5),mPEG-P(LP10-coLC10)(NG10-10),and mPEG-P(LP10-co-LC15)(NG10-15).The three nanogels shared similar surface charge and reductionresponsive behavior,but they had distinct diameters and different drug release profiles.Among them,NG10-5,which has the smallest diameter,was preferentially internalized by tumor cells in vitro and showed rapid migration to the tumor site in vivo.Using doxorubicin(DOX)as a model chemotherapeutic agent,NG10-5/DOX had the most prolonged blood circulation period and highest tumor accumulation after intravenous administration.NG10-5/DOX also had the most potent antitumor effect of all three drug-loaded nanogels.Accordingly,adjusting physicochemical characteristics by changing the amino acid composition might improve the therapeutic efficacies of nanogels and enhance their potential for clinical application.

关 键 词：polypeptide nanogel cystine proportion fate of nanocarrier controlled drug delivery cancer therapy 

分 类 号：TQ460.4[化学工程—制药化工] TB383.1[一般工业技术—材料科学与工程]